Abstract
A series of palladium complexes with 2,2’-bipyridine and 1-(substituted benzyl) azetidine- 3, 3-dicarboxylates as ligands were synthesized and characterized by IR, 1H-NMR, ESI-MS spectra and elemental analysis. The in vitro cytotoxicity assays were carried out against A549, HCT-116, HepG-2 and SGC7901 cancer cell lines. The result showed that most of the complexes possessed moderate antiproliferative activity against HCT-116, HepG-2 and SGC7901 cell lines. Complex 12 (with 2,2’-bipyridine and 1-(3-methoxylbenzyl)azetidine-3,3-dicarboxylate as ligand) was the most potent antitumor agent among all thirteen complexes, which showed comparable or better cytotoxicity against all four tested cancer cell lines than carboplatin. The interaction between complex 12 and pET22b plasmid DNA was investigated by agarose gel electrophoresis, and the result of the study showed that complex 12 had no obvious interaction with the plasmid DNA.
Keywords: Antitumor activity, palladium (II) complex, DNA interaction, 2, 2’-bipyridine, 1-(substituted benzyl) azetidine-3, 3- dicarboxylates, agarose gel electrophoresis.
Graphical Abstract
Medicinal Chemistry
Title:Design, Synthesis and Biological Evaluation of Palladium (II) Complexes with 1-(substituted benzyl) azetidine-3,3-dicarboxylates as Leaving Group
Volume: 11 Issue: 7
Author(s): Gang Xu, Hua Lu, Jiang Zhitao, Shuying Zhang and Shaohua Gou
Affiliation:
Keywords: Antitumor activity, palladium (II) complex, DNA interaction, 2, 2’-bipyridine, 1-(substituted benzyl) azetidine-3, 3- dicarboxylates, agarose gel electrophoresis.
Abstract: A series of palladium complexes with 2,2’-bipyridine and 1-(substituted benzyl) azetidine- 3, 3-dicarboxylates as ligands were synthesized and characterized by IR, 1H-NMR, ESI-MS spectra and elemental analysis. The in vitro cytotoxicity assays were carried out against A549, HCT-116, HepG-2 and SGC7901 cancer cell lines. The result showed that most of the complexes possessed moderate antiproliferative activity against HCT-116, HepG-2 and SGC7901 cell lines. Complex 12 (with 2,2’-bipyridine and 1-(3-methoxylbenzyl)azetidine-3,3-dicarboxylate as ligand) was the most potent antitumor agent among all thirteen complexes, which showed comparable or better cytotoxicity against all four tested cancer cell lines than carboplatin. The interaction between complex 12 and pET22b plasmid DNA was investigated by agarose gel electrophoresis, and the result of the study showed that complex 12 had no obvious interaction with the plasmid DNA.
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Cite this article as:
Xu Gang, Lu Hua, Zhitao Jiang, Zhang Shuying and Gou Shaohua, Design, Synthesis and Biological Evaluation of Palladium (II) Complexes with 1-(substituted benzyl) azetidine-3,3-dicarboxylates as Leaving Group, Medicinal Chemistry 2015; 11 (7) . https://dx.doi.org/10.2174/1573406411666150504123415
DOI https://dx.doi.org/10.2174/1573406411666150504123415 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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